5690-03-9 Usage
Description
Splitomicin is a cell-permeable and selective inhibitor of NAD+-dependent deacetylase activity of the Sir2 protein, with an IC50 value of 60 μM. It is a benzochromenone derivative that creates a phenocopy of the sir2 deletion mutant in S. cerevisiae and sensitizes mammalian cells to various DNA-damaging agents by abrogating Sir2p activity on p53. Splitomicin is known to act by either altering or blocking access to the acetylated histone-binding pocket. It is a potent and selective inhibitor of Sir2, which makes it a promising candidate for various applications, particularly in the field of anti-inflammatory and cancer research.
Uses
Used in Anti-inflammatory Applications:
Splitomicin is used as an anti-inflammatory agent for its ability to selectively and potently inhibit the Sir2 protein, which in turn produces an inhibitory effect on neutrophils. This property makes it a valuable compound in the development of treatments for various inflammatory conditions.
Used in Cancer Research:
In the field of cancer research, Splitomicin is used as a selective and potent inhibitor of Sir2 for its potential to sensitize mammalian cells to a variety of DNA-damaging agents by abrogating Sir2p activity on p53. This characteristic makes it a promising candidate for the development of novel cancer therapeutics, particularly in combination with conventional DNA-damaging agents to enhance their efficacy.
Used in Drug Delivery Systems:
To improve the delivery, bioavailability, and therapeutic outcomes of Splitomicin, researchers are exploring the development of novel drug delivery systems. These systems may involve the use of various organic and metallic nanoparticles as carriers for Splitomicin, aiming to enhance its overall effectiveness in targeting cancer cells and reducing inflammation.
Synthesis Reference(s)
Journal of the American Chemical Society, 69, p. 2341, 1947 DOI: 10.1021/ja01202a027
Biological Activity
Inhibitor of Sir2p (IC 50 = 60 μ M), an NAD + -dependent Sir2 family deacetylase required for chromatin-dependent silencing in yeast.
Biochem/physiol Actions
Cell permeable: yes
Check Digit Verification of cas no
The CAS Registry Mumber 5690-03-9 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 5,6,9 and 0 respectively; the second part has 2 digits, 0 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 5690-03:
(6*5)+(5*6)+(4*9)+(3*0)+(2*0)+(1*3)=99
99 % 10 = 9
So 5690-03-9 is a valid CAS Registry Number.
InChI:InChI=1/C13H10O2/c14-13-8-6-11-10-4-2-1-3-9(10)5-7-12(11)15-13/h1-5,7H,6,8H2
5690-03-9Relevant articles and documents
Organocatalyst-Mediated Dynamic Kinetic Enantioselective Acylation of 2-Chromanols
Glazier, Daniel A.,Schroeder, John M.,Liu, Jitian,Tang, Weiping
supporting information, p. 4646 - 4649 (2018/11/10)
We recently developed a novel chiral catalyst-directed dynamic kinetic diastereoselective acylation of hemiacetals for the synthesis of carbohydrates. In this update, we describe a catalytic method for the dynamic kinetic enantioselective acylation of 2-c
IODOARENE DERIVATIVE, METHOD FOR PRODUCING OPTICALLY ACTIVE SPIROLACTONE COMPOUND USING SAME, AND METHOD FOR PRODUCING OPTICALLY ACTIVE CYCLIZATION ADDUCT
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Paragraph 0106, (2014/01/23)
An optically active spirolactone compound is highly enantioselectively produced by using an iodoarene derivative which can be synthesized easily and which is not racemized easily. [Solution] A hypervalent iodine compound precursor (iodoarene derivative) w
Anionic alternating copolymerization of epoxide and six-membered lactone bearing naphthyl moiety
Sudo, Atsushi,Zhang, Yuan,Endo, Takeshi
experimental part, p. 619 - 624 (2012/01/13)
This article describes the anionic copolymerization of glycidyl phenyl ether (GPE) and 1,2-dihydro-3H-naphtho[2,1-b]pyran-3-one (DHNP), a six-membered aromatic lactone bearing naphthyl moiety. The copolymerization proceeded in a 1:1 alternating manner, to